The Anti-oxidative Effects of Encapsulated Cysteamine During Mice In Vitro Matured Oocyte/Morula-Compact Stage Embryo Culture Model: a Comparison of High-Efficiency Nanocarriers for Hydrophilic Drug Delivery-a Pilot Study.

Although it is well-recognized that antioxidant nano-encapsulation has many benefits such as minimizing side effects (e.g., high-dose toxicity), the most attention was paid to the hydrophobic antioxidant not hydrophilic. In this regard, we sought to compare two hydrophilic model nanocarriers to deliver the optimal dose of cystamine (Cys) into the in vitro matured oocyte and the first cleavage stages until morula-compact stage embryonic cells. The formation of Cys-loaded solid self-emulsifying lipid (Cys + SLN) and Cys-loaded chitosan shell (Cys-CS-NC) were confirmed by FT-IR and UV-Vis spectrophotometry, dynamic light scattering (DLS), transmission electron microscopy (TEM), and scanning electron microscopy (SEM) technologies. In two experiments, the oocytes/presumptive zygotes were cultured under various concentrations of Cys-SLN and Cys-CS-NC. The results of nuclear staining (aceto-orcein and Hoechst 33342), H2DCFDA fluorescent staining, chemiluminescence test, and quantitative reverse transcription-PCR (qRT-PCR) technique as in vitro toxicity studies demonstrated that adding the lowest dose of Cys-encapsulated in both nanocarriers [Cys-SLN (5 µM) and Cys-CS-NC (10 µM)] to maturation or culture medium could accumulate a strong anti-oxidative effect in oocyte/embryo by controlled release and enhanced intracellular penetration of Cys. In comparison, Cys-SLN (5 µM) is more effective than Cys-CS-NC (10 µM) groups to improve the expression of antioxidant genes (SOD, CAT, GPx) or anti-apoptotic (BCL-2) gene and decreased apoptosis (BAX and caspase-3) or intra-/extracellular ROS levels. In a nutshell, both nanocarriers (CS-NC or SLN) can deliver the lowest dose of Cys into the oocyte/embryo, thus encouraging a better expansion of antioxidant genes and enhancing the development of in vitro oocyte/embryo.

Solidification to improve the biopharmaceutical performance of SEDDS: Opportunities and challenges.

Self-emulsifying drug delivery systems (SEDDS) offer potential for overcoming the inherent slow dissolution and poor oral absorption of hydrophobic drugs by retaining them in a solubilised state during gastrointestinal transit. However, the promising biopharmaceutical benefits of liquid lipid formulations has not translated into widespread commercial success, due to their susceptibility to long term storage and in vivo precipitation issues. One strategy that has emerged to overcome such limitations, is to combine the solubilisation and dissolution enhancing properties of lipids with the stabilising effects of solid carrier materials. The development of intelligent hybrid drug formulations has presented new opportunities to harness the potential of emulsified lipids in optimising oral bioavailability for lipophilic therapeutics. Specific emphasis of this review is placed on the impact of solidification approaches and excipients on the biopharmaceutical performance of self-emulsifying lipids, with findings highlighting the key design considerations that should be implemented when developing hybrid lipid-based formulations.

Comparative in vitro intestinal digestion of 1,3-diglyceride and 1-monoglyceride rich oils and their mixtures.

Intestinal in vitro digestion of 1,3-diolein (DO), 1-monoolein (MO), DO:MO (1:1) rich oils, and triolein (TO), was performed to study the rate and extent of hydrolysis as well as their bioaccessibility in detail, with special emphasis on 1,3-DO and 1-MO forms, as potential bioactive lipids with additional technological functions such as self-emulsifying lipids. The importance of in vitro conditions on non-desirable acylmigration was also shown. The rate of in vitro intestinal lipolysis was in increasing order TO95%) of DO, MO and DO:MO were found within the micellar phase fraction during digestion, suggesting a high bioaccessibility. A positive correlation between the degree of lipolysis and the number of mixed micelles formed at the end of digestion was found. As summary, the obtained results would enhance the selection of glycerides to formulate ingredients with different purposes. Thus, in case a final high level of 1-MO would be desired to take advantage of the bioactivity of 1-MO, oils under the form of DO or DO:MO might be superior to MO. In case a high 1-MO level together with a low 2-MO level would be desired at the same time, mixtures of DO:MO or MO would be preferred. In case a higher self-emulsifying ability would be desired, the preferred forms would be MO and DO:MO. Finally, in case all the potential functionalities would be desired at the same time, namely the highest bioactivity, together with a high self-emulsifying ability, the mixture DO:MO might be suggested as an interesting product, with the additional economical advantage.